Pennefather J N, Gillman T A, Mitchelson F
Department of Pharmacology, Monash University, Clayton, Victoria, Australia.
Eur J Pharmacol. 1994 Sep 12;262(3):297-300. doi: 10.1016/0014-2999(94)90745-5.
The aim of this study was to characterise the muscarinic receptor present in the uterus of the virgin rat. Homogenate binding studies were undertaken using [3H]quinuclidinyl benzilate as the radioligand and atropine (10 microM) to determine non-specific binding. [3H]Quinuclidinyl benzilate binding was saturable with a Kd of 63 pM and a Bmax of 3 fmol/mg protein. The pKi values obtained using antagonists with high affinity for differing muscarinic receptor subtypes were pirenzepine, 6.2; hexahydrosiladifenidol, 6.9; AF-DX 116 (11-[[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]5,11-dihydro-6H - pyrido[2,3-b][1,4]benzodiazepine-6-one), 7.0; and himbacine, 7.8. These findings suggest that muscarinic M2 receptors are present in rat uterus.
本研究的目的是鉴定未交配大鼠子宫中存在的毒蕈碱受体。使用[3H]喹核醇基苯甲酸酯作为放射性配体并使用阿托品（10微摩尔）进行匀浆结合研究，以确定非特异性结合。[3H]喹核醇基苯甲酸酯结合具有饱和性，解离常数（Kd）为63皮摩尔，最大结合量（Bmax）为3飞摩尔/毫克蛋白质。使用对不同毒蕈碱受体亚型具有高亲和力的拮抗剂所获得的抑制常数（pKi）值分别为：哌仑西平，6.2；六甲硅铵，6.9；AF-DX 116（11-[[2-[(二乙氨基)甲基]-1-哌啶基]乙酰基]-5,11-二氢-6H-吡啶并[2,3-b][1,4]苯并二氮杂卓-6-酮），7.0；和辛巴辛，7.8。这些发现表明大鼠子宫中存在毒蕈碱M2受体。
